DRUG TRANSPORT IN THE LIVER - Drug Transporters: Molecular Characterization and Role in Drug Disposition - page 373

TABLE 13.3. Regulation of Transport Proteins a
Transport Induce/ Nuclear

Protein Repress RNA Protein Receptor Ligands Test System Refs.

Ntcp (r) ↑ RAR Retinoids (LG364, TTNPB) HepG2 reporter assay 71

Ntcp (r) ↓ RAR Cytokines (TNF , IL-1 ) HepG2 reporter assay 71

OATP1B3 ↑ FXR Bile acids (CDCA) HepG2 reporter assay 72

MRP1, 2, 3 ↑ CAR Phenobarbital HepG2, Northern blots 155,257

BSEP ↑ ×× FXR Bile acids (CDCA, DCA, LCA,

DKCA)

Human tissue immunoblot,
HepG2 reporter assay

73,258

Mrp2 (r) ↑ RAR Retinoids (LG364, TTNPB) HepG2 reporter assay 71

Mrp2 (r) ↓ RAR Cytokines (TNF , IL-1 ) HepG2 reporter assay 71

MRP2 ↑ ×× PXR Rifampicin, hyperforin,

clotrimazol, rifampin

Human hepatocytes, duodenal
biopsy, HepG2 reporter assays,
RT-PCR, Western blot

75,76,297

MRP2 ↑ × FXR CDCA and GW4064 HepG2 Northern blot 76

MRP2 ↑ ×× CAR Phenobarbital Human hepatocytes 259

MRP3 Slight ↑× PXR Rifampicin HepG2 RT-PCR 297

MRP3 ↑ × PXR Clotrimazole, rifampicin, RU486,

metyrapone, PCN

HebG2, HuH7 298

MRP4 ↑ × CAR Phenobarbital Human hepatocytes, HepG2 260

↑ ×

MRP5 PXR Rifampicin HepG2 RT-PCR 297

↑ ×

MDR1 PXR Rifampin, rifampicin LS174T Northern blot, human

hepatocytes, LS180 cells
Northern blot

74,152

Mrp2 (r) ↑ ×× PXR PCN, spironolactone, DEX Rat hepatocytes, FAO 76,261,262,297,299,300

Mrp2 (r) ↑ × Nrf2 Ethoxyquin, oltipraz in vivo 299

Mrp2 (r) ↑ ×× CAR Phenobarbital Rat hepatocytes, FAO 76,259,297,301